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Nineteen triterpenoids, including five previously unknown (four triucallane-type derivatives and one highly oxidized A, B-seco limonoids), together with fourteen known triterpenoids, were isolated from the fruits of Aphanamixis polystachya. Their structures were elucidated by extensive spectroscopic analysis. All isolates were evaluated their anti-inflammatory activities. The result showed that all compounds inhibit LPS-induced nitric oxide production in RAW264.7 macrophages with their IC50 value ranging from 95 to 1332 uM, and compound 6 exhibited obvious anti-inflammatory activity comparable to that of the positive control, with IC50 values of 94.96 uM.
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Meliaceae , Triterpenos , Frutas/química , Triterpenos/farmacología , Óxido Nítrico , Estructura Molecular , Meliaceae/química , Antiinflamatorios/farmacologíaRESUMEN
OBJECTIVE: To observe the effects of acupuncture on the expression of type â ¢ phosphatidylinositol 3-hydroxykinase (PI3K) and Beclin-1 in hippocampus of rats with cerebral ischemia/reperfusion injury (CI/RI), so as to explore the mechanism of acupuncture in regulating type â ¢ PI3K pathway to activate autophagy in the hippocampal neurons of CI/RI rats. METHODS: SD rats were randomly divided into sham operation group (n=11) and operation group. Then after successful modeling, rats in the operation group were randomly divided into model, acupuncture, model+3-MA and acupuncture+3-MA groups, with 11 rats in each group. The model of CI/RI was established by occlusion of the middle cerebral artery. Rats in the model+3-MA and acupuncture+3-MA groups were injected with 3-MA (400 nmol/ 5 µL) 5 µL into the lateral ventricle 30 min before reperfusion. Rats in the acupuncture and acupuncture+3-MA groups were punctured with filiform needles at "Dazhui" (GV14), "Shuigou" (GV26) and "Baihui" (GV20) and stimulated manually once every 15 min. The acupuncture intervention was conducted for 30 min each time, once every 12 h for a total of 7 times. The degree of neurological impairment was evaluated 2 h after reperfusion and after intervention by Garcia score. After intervention, the percentage of cerebral ischemic area was observed by TTC staining, the protein expression levels of type â ¢ PI3K, Beclin-1, microtubule-associated protein 1 light chain 3B (LC3B), lysosome associated membrane protein 2 (Lamp2) and P62 in ischemic hippocampal tissue were detected by Western blot, the ultrastructure of neurons in ischemic hippocampus was observed by transmission electron microscopy (TEM). RESULTS: Compared with the sham operation group, the Garcia score was decreased (P<0.01), the percentage of cerebral ischemic area was increased (P<0.01), the expression levels of type â ¢ PI3K, Beclin-1, LC3B-â ¡/â , Lamp2 proteins were decreased (P<0.01), and the expression level of P62 protein was increased (P<0.01) in ischemic hippocampal tissue in the model group. Compared with the model group, the Garcia score was increased (P<0.01), the percentage of cerebral ischemic area was decreased (P<0.01), the expression levels of type â ¢ PI3K, Beclin-1, LC3B-â ¡/â , Lamp2 proteins were increased (P<0.01, P<0.05) and the expression level of P62 was decreased (P<0.01) in ischemic hippocampal tissue in the acupuncture groupï¼ the percentage of cerebral ischemic area was increased (P<0.05), the expressions of type â ¢ PI3K and Beclin-1 were decreased (P<0.01) and the expression level of P62 protein was increased (P<0.05) in ischemic hippocampal tissue in the mo-del+3-MA group. Compared with the model +3-MA group, the Garcia score was increased (P<0.05), the percentage of cerebral ischemic area was decreased (P<0.01), the expression levels of type â ¢ PI3K, Beclin-1, LC3B-â ¡/â in ischemic hippo-campal tissue were increased (P<0.01, P<0.05) in the acupuncture+3-MA group. Compared with the acupuncture group, the Garcia score was decreased, the percentage of cerebral ischemic area was increased (P<0.05, P<0.01), the expression levels of type â ¢ PI3K, Beclin-1, Lamp2 proteins were decreased (P<0.01, P<0.05) and P62 protein was increased (P<0.05) in ischemic hippocampal tissue in the acupuncture+3-MA group. The results of TEM showed that the edema of neurons was heavier, and few hypolysosomes existed in the model group; there was no obvious damage to neuronal structure, intracellular matrix was abundant, and a few lysosomes existed in the acupuncture group; the neuronal cells had mild edema and primary lysosomes were present in the acupuncture +3-MA group. CONCLUSION: Acupuncture can improve the symptoms of neurological impairment and reduce the percentage of cerebral ischemic area in rats with CI/RI. The mechanism may be related to regulating type â ¢ PI3K/Beclin-1 pathway, up-regulating the expressions of autophagy related factors LC3B-â ¡ and Lamp2, and down-regulating the expression of P62.
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Terapia por Acupuntura , Isquemia Encefálica , Daño por Reperfusión , Ratas , Animales , Ratas Sprague-Dawley , Beclina-1/genética , Fosfatidilinositol 3-Quinasas/genética , Isquemia Encefálica/genética , Isquemia Encefálica/terapia , Infarto Cerebral , Hipocampo , Daño por Reperfusión/genética , Daño por Reperfusión/terapia , Neuronas , Autofagia/genética , ReperfusiónRESUMEN
In this work, the differences in macrostructure and microstructure, rheology, and storage stability of pre-emulsified safflower oil (PSO) prepared by natural and magnetic field modified soy 11S globulin were analysised. It was concluded that the PSO with magnetic field modified soy 11S globulin (MPSO) has better emulsifying activity and physical stability. The changes in gel quality, oxidational sensitivity, rheological, and sensory properties of pork batters with different substitute ratios (0%, 25%, 50%, 75%, and 100%) of pork back-fat by MPSO with magnetic field modified soy 11S globulin were studied. Compared to the sample without MPSO, pork batter with MPSO showed higher emulsion stability, apparent viscosity, Lâ value, springiness, cohesiveness, and expressible moisture, while lower aâ value and cooking loss. Moreover, added MPSO could be more uniformly distributed into the meat matrix with smaller holes. With the increase in the replacement proportion of pork back-fat, the hardness, water- and fat-holding capacity, and P21 of pork batter significantly decreased (P < 0.05). As revealed by sensory evaluation and TBARS, using MPSO to substitute for pork back-fat decreased the lipid oxidational sensitivity of pork batter, and without negative effects on the appearance, juiciness and overall acceptability. Overall, it is feasible to apply MPSO as a pork-fat replacer to produce reduced-animal fat pork batter with excellent gel and sensory properties.
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Sustitutos de Grasa , Globulinas , Carne de Cerdo , Carne Roja , Animales , Porcinos , Manipulación de Alimentos , Aceite de Cártamo , Sustitutos de Grasa/química , Reología , Campos MagnéticosRESUMEN
Lotus (Nelumbo nucifera Gaertn.) is a well-known food and medicinal plant. Lotus seedpod (Receptaculum Nelumbinis) is the by-products during lotus products processing, which is considered as waste. Numerous studies have been conducted on its phytochemicals, biological activity and industrial application. However, the information on lotus seedpod is scattered and has been rarely summarized. In this review, summaries on preparation and identification of phytochemicals, the biological activities of extracts and phytochemicals, and applications of raw material, extracts and phytochemicals for lotus seedpod were made. Meanwhile, the future study trend was proposed. Recent evidence indicated that lotus seedpods extracts, obtained by non-organic and organic solvents, possessed several activities, which were influenced by extraction solvents and methods. Lotus seedpods were rich in phytochemicals categorized as different chemical groups, such as proanthocyanidins, oligomeric procyanidins, flavonoids, alkaloids, terpenoids, etc. These phytochemicals exhibited various bioactivities, including ameliorating cognitive impairment, antioxidation, antibacterial, anti-glycative, neuroprotection, anti-tyrosinase and other activities. Raw material, extracts and phytochemicals of lotus seedpods could be utilized as sources for biochar and biomass material, in food industry and as dye. This review gives well-understanding on lotus seedpod, and provides theoretical basis for its future research and application.
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Qishen Yiqi Dripping Pills(QSYQ) are used clinically to treat various myocardial ischemic diseases, such as angina pectoris, myocardial infarction, and heart failure; however, the molecular mechanism of QSYQ remains unclear, and the scientific connotation of traditional Chinese medicine(TCM) compatibility has not been systematically explained. The present study attempted to screen the critical pathway of QSYQ in the treatment of myocardial ischemia by network pharmacology and verify the therapeutic efficacy with the oxygen-glucose deprivation(OGD) model, in order to reveal the molecular mechanism of QSYQ based on the critical pathway. The key targets of QSYQ were determined by active ingredient identification and target prediction, and underwent pathway enrichment analysis and functional annotation with David database to reveal the biological role and the critical pathway of QSYQ. Cell counting Kit-8(CCK-8), lactate dehydrogenase(LDH), and Western blot tests were launched on high-content active ingredients with OGD cell model to reveal the molecular mechanism of QSYQ based on the critical pathway. The results of network pharmacology indicated that QSYQ, containing 18 active ingredients and 82 key targets, could protect cardiomyocytes by regulating biological functions, such as nitric oxide biosynthesis, apoptosis, inflammation, and angiogenesis, through TNF signaling pathway, HIF-1 signaling pathway, PI3 K-Akt signaling pathway, etc. HIF-1 signaling pathway was the critical pathway. As revealed by CCK-8 and LDH tests, astragaloside â £, salvianic acid A, and ginsenoside Rg_1 in QSYQ could enhance cell viability and reduce LDH in the cell supernatant in a concentration-dependent manner(P<0.05). As demonstrated by the Western blot test, astragaloside â £ significantly down-regulated the protein expression of serine/threonine-protein kinase(Akt1) and hypoxia-inducible factor 1α(HIF-1α) in the HIF-1 signaling pathway, and up-regulated the protein expression of vascular endothelial growth factor A(VEGFA). Salvianic acid A significantly down-regulated the protein expression of upstream phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha(PIK3 CA) and downstream HIF-1α of Akt1. Ginsenoside Rg_1 significantly down-regulated the expression of HIF-1α protein and up-regulated the expression of VEGFA. The therapeutic efficacy of QSYQ on myocardial ischemia was achieved by multiple targets and multiple pathways, with the HIF-1 signaling pathway serving as the critical one. The active ingredients of QSYQ could protect cardiomyocytes synergistically by regulating the targets in the HIF-1 signaling pathway to inhibit its expression.
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Medicamentos Herbarios Chinos , Isquemia Miocárdica , Medicamentos Herbarios Chinos/farmacología , Humanos , Subunidad alfa del Factor 1 Inducible por Hipoxia/genética , Isquemia Miocárdica/tratamiento farmacológico , Isquemia Miocárdica/genética , Transducción de Señal , Factor A de Crecimiento Endotelial VascularRESUMEN
BACKGROUND: Breast cancer (BC) has the highest morbidity and the fifth-highest mortality rate among women in China. Peritoneal metastases from BC are rare, and presently, there are no guidelines or international consensus on its treatment. Patients with a prognosis of peritoneal carcinomatosis (PC) have poorer survival rates than patients with other regional metastases from BC. METHODS: Four BC PC patients, who had undergone cytoreductive surgery (CRS) + hyperthermic intraperitoneal chemotherapy (HIPEC), participated in this study. Clinicopathologic characteristics and overall survival (OS) data were collected and analyzed. RESULTS: Patients' average age when they underwent CRS + HIPEC was 59.8 years. The average time of CRS + HIPEC was 8.8 h. The median number of resected organ areas was 7. Following CRS + HIPEC, each of the 4 patients survived for 31, 28, 16 and 52 months, respectively. There were no serious adverse events during the perioperative period. CONCLUSIONS: The study examined the detailed process of CRS + HIPEC and found that patients with BC PC may benefit from this treatment. The 4 cases provided evidence that the integrated therapy of CRS + HIPEC is a promising strategy that could improve outcomes for BC PC patients. Further, no serious adverse events (SAEs) occurred during the CRS + HIPEC perioperative period.
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Two new sesquiterpenoids, including a kessane-type sesquiterpenoid (1) and one bisabolane derivative (2), together with fourteen known sesquiterpenoids (3-16), were isolated from the roots and rhizomes of Valeriana amurensis. The structures of new compounds were established on the basis of extensive spectroscopic analysis. All isolates were evaluated for their effects on nerve growth factor (NGF)-mediated neurite outgrowth in pheochromocytoma (PC12) cells. As a results, four compounds including 10-12 and 15 showed potent promoting effects at the concentration of 10 µM on NGF-induced neurite outgrowth in PC12 cells with the differentiation rate of 11.84%, 12.21%, 13.77% and 12.16%, respectively.
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Factor de Crecimiento Nervioso/farmacología , Proyección Neuronal/efectos de los fármacos , Raíces de Plantas/química , Rizoma/química , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología , Valeriana/química , Animales , Espectroscopía de Resonancia Magnética con Carbono-13 , Factor de Crecimiento Nervioso/metabolismo , Células PC12 , Espectroscopía de Protones por Resonancia Magnética , Ratas , Sesquiterpenos/químicaRESUMEN
AIMS/INTRODUCTION: To explore relationships between polyunsaturated fatty acids (PUFA) and non-alcoholic fatty liver disease (NAFLD) in patients with type 2 diabetes, and whether insulin action has an interactive effect with PUFA on NAFLD progression. MATERIALS AND METHODS: We extracted clinical and omics data of 482 type 2 diabetes patients from a tertiary hospital consecutively from April 2018 to April 2019. NAFLD was estimated by ultrasound at admission. Plasma fasting n3 and n6 fatty acids were quantified by liquid chromatography-tandem mass spectrometry analysis. Restricted cubic spline nested in binary logistic regression was used to select the cut-off point, and estimate odds ratios and 95% confidence intervals. Additive interactions of the n6 : n3 ratio with insulin action for NAFLD were estimated using relative excess risk due to interaction, attributable proportion due to interaction and synergy index. Relative excess risk due to interaction >0, attributable proportion due to interaction >0 or synergy index >1 indicates biological interaction. Spearman correlation analysis was used to obtain partial correlation coefficients between PUFA and hallmarks of NAFLD. RESULTS: Of 482 patients, 313 were with and 169 were without NAFLD. N3 ≥800 and n6 PUFA ≥8,100 µmol/L were independently associated with increased NAFLD risk; n6 : n3 ratio ≤10 was associated with NAFLD (odds ratio 1.80, 95% confidence interval 1.20-2.71), and the effect size was amplified by high C-peptide (odds ratio 8.89, 95% confidence interval 4.48-17.7) with significant interaction. The additive interaction of the n6 : n3 ratio and fasting insulin was not significant. CONCLUSION: Decreased n6 : n3 ratio was associated with increased NAFLD risk in type 2 diabetes patients, and the effect was only significant and amplified when there was the co-presence of high C-peptide.
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Péptido C/sangre , Diabetes Mellitus Tipo 2/sangre , Ácidos Grasos Omega-3/sangre , Ácidos Grasos Omega-6/sangre , Enfermedad del Hígado Graso no Alcohólico/sangre , Anciano , Estudios Transversales , Diabetes Mellitus Tipo 2/complicaciones , Femenino , Humanos , Pacientes Internos/estadística & datos numéricos , Insulina/sangre , Masculino , Persona de Mediana Edad , Enfermedad del Hígado Graso no Alcohólico/etiología , Oportunidad RelativaRESUMEN
Objective To explore the optimal therapy time for the treatment of severe coronavirus disease 2019(COVID-19)by traditional Chinese medicine(TCM)and its influence on the therapeutic effect and prognosis. Methods The clinical data,laboratory findings,and outcomes of 64 patients with severe COVID-19 treated with TCM and western medicine in Chongqing from January 20,2020, to March 11,2020 were retrospectively analyzed.Patients were divided into early intervention group[TCM was initiated within 3 days (including day 3) after the first diagnosis of severe type/critical type COVID-19]and late intervention group[TCM was initiated after 7 days (including day 7) after the first diagnosis of severe type /critical type COVID-19].The changes in clinical parameters during the course of disease were compared between the two groups. Results On day 14,the oxygenation index was 292.5(252.0,351.0)mmHg in the early intervention group,which was significantly higher than that in the late intervention group [246.0(170.0,292.5)mmHg](P=0.005).The length of hospital stay [(18.56±1.11)d vs.(24.87±1.64)d,P=0.001],duration of ICU stay [(14.12±0.91)d vs.(20.00±1.53)d,P=0.000] and time to negativity [(16.77±1.04)d vs.(22.48±1.66)d,P=0.001] in the early intervention group were significantly shorter than those in the late intervention group.The intubation rate(7.3%)in the early intervention group was significantly lower than that in the late intervention group(30.4%)(P=0.028). Conclusion Early TCM therapy within three days after a diagnosis of severe COVID-19 can shorten the length of hospital stay,duration of ICU stay,and time to negativity and decrease intubation rate.
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Betacoronavirus , Infecciones por Coronavirus , Medicina Tradicional China , Pandemias , Neumonía Viral , COVID-19 , Infecciones por Coronavirus/tratamiento farmacológico , Humanos , Neumonía Viral/tratamiento farmacológico , Pronóstico , Estudios Retrospectivos , SARS-CoV-2 , Tratamiento Farmacológico de COVID-19RESUMEN
The combination of enzymolysis of compound enzyme, oxidation of sodium hypochlorite, and cationic etherification of 3-chloro-2-hydroxypropyl trimethyl ammonium chloride (CHPTMA) was selected for the functionalization of rice starch (RS) to better raise the performances. The results showed that the oxidation and etherification could improve the acid and alkali resistance of RS, and enhanced its thermal stability. The crystalline structure of RS was an A-type, the enzymolysis, oxidation, and etherification did not change the structural type, while the crystallinity degree of RS derivatives was all reduced. The enzymolysis, oxidation, and etherification altered the pasting properties of RS, and could effectively decrease the setback and breakdown of RS. The oxidation of sodium hypochlorite not only damaged RS particles containing no micropores, but also destroyed the particles containing the micropores. The enzymolysis and oxidation more seriously destroyed the crystalline region than cationic etherification. The oxidation could increase the enthalpy change of RS, whereas the enzymolysis and etherification decreased its enthalpy change. In addition, the enzymolysis and oxidation could lead to the evident increase in average size of RS. The cationic etherification was able to improve the adsorption of Cu2+ on RS, whereas the low oxidation could only slightly ameliorate the adsorption of Cu2+ . PRACTICAL APPLICATION: Cationic oxidized microporous rice starch as an adsorbent, slow-release agent, and flocculant will be well used in food, medicine, pesticide, papermaking, waste water treatment, and so on owing to its abundant micropores, anionic groups, and cationic groups as well as small particle size and narrow size range.
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Oryza/química , Extractos Vegetales/química , Almidón/química , Cationes/química , Oxidación-Reducción , Tamaño de la Partícula , Termodinámica , AguaRESUMEN
Wogonin is a main effective component of Scutellaria baicalensis, with a significant anti-cancer activity. Recently, extensive studies focused on anti-cancer pharmacological effects of wogonin, but there were still a few studies on its molecular mechanism. Therefore, the molecular targets of its anti-cancer activity were still unclear. In this study, network pharmacology was applied to investigate the potential targets and molecular pathway of wogonin in inhibiting the growth of colorectal cancer. It indicated that Wnt/ß-catenin was a key pathway of wogonin on colorectal cancer. Then, pharmacology and molecular mechanism studies were performed according to network pharmacological results. Pharmacological results revealed that wogonin inhibited significantly the proliferation of SW480(P<0.001), with a concentration-dependent regularity in the range of 12.5-50 µmol·L~(-1). Additionally, wogonin could induce G_1 phase blocking of SW480 cells. Western blot was used to investigate the effect of wogonin on four characteristic proteins of Wnt/ß-catenin pathway. CTNNB1(ß-catenin), BIRC5(survivin) and GSK3 B were down-regulated significantly, while the expression level of BAX was up-regulated(P<0.05). In conclusion, wogonin could inhibit the proliferation of SW480 cells through Wnt/ß-catenin pathway. The feature protein CTNNB1(ß-catenin), BIRC5(survivin), GSK3 B and BAX were identified as the potential targets. This study illuminated the anti-cancer molecular mechanism and drug targets of wogonin, which provided a theoretical basis for anti-colon cancer drug discovery and clinical application.
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Neoplasias Colorrectales , Glucógeno Sintasa Quinasa 3 , Línea Celular Tumoral , Proliferación Celular , Flavanonas , Humanos , Vía de Señalización Wnt , beta CateninaRESUMEN
The research on biopharmaceutics classification system of Chinese materia medica( CMMBCS) should be finally implemented to the holistic research level of traditional Chinese medicine compounds,while the overall biopharmaceutical properties of traditional Chinese medicine compounds are not only the sum of solubility and permeability of each component. In this study,Gegen Qinlian Tablets was used as the research object,and the contents of 12 representative components,i.e. puerarin,daidzin,baicalin,daidzein,wogonoside,baicalein,wogonin,glycyrrhizic acid,coptisine hydrochloride,epiberberine,berberine hydrochloride and palmatine hydrochloride,were simultaneously determined by HPLC to obtain the mass weight of each component. The in vitro lipopolysaccharide( LPS)-induced RAW264. 7 cells inflammation model was established to investigate the anti-inflammatory effects of 12 representative components and obtain the efficacy weight of each component. In order to obtain the number of doses and effective permeability coefficient which can represent the overall biopharmaceutical properties of Gegen Qinlian Tablets,mass weight was combined with efficacy weight to integrate the solubility and permeability data of each component determined by typical shake flask method and in situ single pass intestinal perfusion model respectively. The results indicated that Gegen Qinlian Tablets should be categorized â £ drug of the CMMBCS with low solubility and low permeability.
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Antiinflamatorios/farmacología , Biofarmacia/clasificación , Medicamentos Herbarios Chinos/clasificación , Materia Medica/clasificación , Medicamentos Herbarios Chinos/farmacología , ComprimidosRESUMEN
A chemical investigation on 70% EtOH extract from the bark of Phellodendron chinense Schneid (Rutaceae) led to six new methyl apiofuranosides (1-6), and ten known compounds (7-16). All these compounds were characterized by the basic analysis of the spectroscopic data including extensive 1D-, 2D-NMR (HSQC, HMBC), and high-resolution mass spectrometry, and the absolute configurations were determined by both empirical approaches and NOESY. Inhibitory effects of compounds 1-9 and 11-16 on nitric oxide production were investigated in lipopolysaccharide (LPS)-mediated RAW 264.7 cells, as a result, most of these isolates inhibited nitric oxide (NO) release, and among them 9, 11, and 12 displayed the strongest inhibition on NO release at the concentration of 12.5 µM.
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Lipopolisacáridos/efectos adversos , Óxido Nítrico/metabolismo , Pentosas/farmacología , Phellodendron/química , Animales , Ratones , Estructura Molecular , Pentosas/química , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Células RAW 264.7RESUMEN
A new isobenzofuranone derivative has been isolated from Phlomis betonicoides by using various chromatographic techniques, including silica gel, Sephadex LH-20, MCI-gel resin and RP-HPLC. This compound was determined as 5-(3-hydroxypropyl)-2,2-dimethyl-2H-furo[3,4-h]chromen-7(9H)-one (1) by NMR, MS, IR and UV spectroscopic data. Compound 1 showed potent antibacterial activity with an MIC90 value of (58.4 ± 4.2) mg·L⻹ for methicillin resistant Staphylococcus aureus (MRSA) strain [levofloxacin as a control with MIC90 value of (52.8±4.6) mg·L⻹].
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Antibacterianos/farmacología , Benzofuranos/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Phlomis/química , Antibacterianos/aislamiento & purificación , Benzofuranos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacologíaRESUMEN
To illustrate the intrinsic dissolution rate(IDR) involved in biopharmaceutics classification system of Chinese materia medica(CMMBCS), investigate the effect of artificial multicomponent environment on IDR of berberine, by using a non-disintegrating disk, and summarize related rules by using the obtained data. Progressive levels design was used to investigate the effects of single component environment (puerarin, baicalin, and glycyrrhizic acid); double-component environment(puerarin+baicalin, puerarin+ glycyrrhizic acid, baicalin+glycyrrhizic acid); and triple-component environment(puerarin+baicalin+glycyrrhizic acid) on IDR of berberine, laying a foundation for further researches on the absorption mechanism of multiple components.
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Berberina/química , Medicamentos Herbarios Chinos/química , Materia Medica , Biofarmacia , SolubilidadRESUMEN
Nine dimeric acylphloroglucinols, including the new hyperjaponicols A-D (1-4), were isolated from the whole plant of Hypericum japonicum. The new structures were determined by the interpretation of NMR and MS data, and the relative configuration of the known compound, sarothralen C (5), was reassigned via NMR spectroscopic analysis and single-crystal X-ray diffraction data. The inhibitory activities of the isolates against four bacterial strains were evaluated, and compounds 1-4, 6, and 7 exhibited significant antibacterial activity with MIC values of 0.8-3.4 µM. In addition, compound 3 showed moderate lipase inhibitory activity (IC50 8.3 µM).
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Antibacterianos/química , Hypericum/química , Floroglucinol/química , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética/métodos , Difracción de Rayos X/métodosRESUMEN
One of the advantages of biopharmaceutics classification system of Chinese materia medica (CMMBCS) is expanding the classification research level from single ingredient to multi-components of Chinese herb, and from multi-components research to holistic research of the Chinese materia medica. In present paper, the alkaloids of extract of huanglian were chosen as the main research object to explore their change rules in solubility and intestinal permeability of single-component and multi-components, and to determine the biopharmaceutical classification of extract of Huanglian from holistic level. The typical shake-flask method and HPLC were used to detect the solubility of single ingredient of alkaloids from extract of huanglian. The quantitative research of alkaloids in intestinal absorption was measured in single-pass intestinal perfusion experiment while permeability coefficient of extract of huanglian was calculated by self-defined weight coefficient method.
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Medicamentos Herbarios Chinos/química , Materia Medica/clasificación , Extractos Vegetales/química , Animales , Biofarmacia , Medicamentos Herbarios Chinos/clasificación , Absorción Intestinal , Extractos Vegetales/clasificaciónRESUMEN
Six new highly oxygenated grayanane diterpenoids, neopierisoids G-L, 1-6, together with 10 known related compounds, 7-16, were identified from the flowers of the poisonous plant Pieris japonica. The structures were elucidated on the basis of comprehensive NMR spectroscopy and mass analysis. The relative configurations of 1-6 were elucidated by analysis of ROESY spectra and comparison of NMR data with the analogues. The absolute configurations of 1-6 were established by the X-ray diffraction analysis of 1 and comparison of the CD spectra of 1-6. Compared with the skeleton of the normal grayanane diterpenoids, compounds 1-6 shared an unusual seco A ring moiety. The antifeedant activities of compounds 1-16 against Pieris brassicae were evaluated by using a dual-choice bioassay, and compounds 1-10 with a normal grayanane skeleton showed potent antifeedant activity against P. brassicae. The structure-activity relationships of antifeedant activities of 1-16 against P. brassicae are discussed.
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Mariposas Diurnas/efectos de los fármacos , Diterpenos/química , Diterpenos/farmacología , Ericaceae/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Animales , Mariposas Diurnas/fisiología , Conducta Alimentaria/efectos de los fármacos , Flores/química , Estructura Molecular , Relación Estructura-ActividadRESUMEN
BACKGROUND: This study aims to assess the diagnostic and prognostic value of Swansea criteria in diagnosing acute fatty liver of pregnancy (AFLP) in a Chinese population. METHODS: A retrospective study was conducted on 52 Chinese women diagnosed with AFLP. All selected cases were reassessed using the Swansea criteria with special focus on the noninvasive criteria, since performing a liver biopsy for this indication is rare in a Chinese population. RESULTS: Ninety point four percent of patients fulfilled five or more of the Swansea criteria. Thirty-one cases were positive for six or more Swansea criteria, but there were no significance differences between patients when using a cutoff criteria <6 or >6. When patients were positive for less than seven criteria, frequency of stillbirth, continuous blood purification (CBP) treatment, hysterectomy, and postpartum hemorrhage were not increased. However, patients who were positive for seven or more criteria had a significantly higher risk of stillbirth and a higher rate of CBP treatment (p < 0.05). Areas under the receiver operating characteristic (ROC) curve of postpartum hemorrhage was 0.670, which reached a statistical significance (p = 0.040). We observed a significantly elevated postpartum hemorrhage along with positivity of the Swansea criteria (p = 0.040). CONCLUSIONS: Swansea criteria without liver biopsy are good screening tools for AFLP diagnosis, and may be useful for assessing disease severity.
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Hígado Graso/diagnóstico , Medicina Tradicional China/métodos , Complicaciones del Embarazo/diagnóstico , Diagnóstico Prenatal/métodos , Adulto , China , Diagnóstico Diferencial , Diagnóstico Precoz , Femenino , Edad Gestacional , Humanos , Pruebas de Función Hepática/métodos , Embarazo , Estudios Retrospectivos , Sensibilidad y Especificidad , Adulto JovenRESUMEN
Hyperjapones A-E (1-5), novel terpenoid polymethylated acylphloroglucinols (TPAPs) with unusual architectures, were characterized from Hypericum japonicum. Their structures and absolute configurations were determined by comprehensive spectroscopic data and X-ray diffractions. Compound 1 was obtained as a racemic mixture and was separated by a column coated with cellulose tris(4-methylbenzoate) after attempts with various chiral materials. Compounds 1, 2, and 4 exhibited moderate antitumor activities in vitro.